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Benzodiazepine Receptors

  • Richard F. Squires

Abstract

The author’s interest in benzodiazepine (BZ) receptors was aroused by a report1 that a series of BZs displaced [3H]strychnine from specific binding sites on membranes from rat brainstem and spinal cord with good correlations between the potencies of the BZs in displacing [3H]strychnine in vitro, and in in vivo pharmacological tests predictive of clinical efficacy. Candace Pert introduced me to affinity binding methodology in 1972. In December, 1974, at a benzo diazepine symposium,2 strong biochemical3 and electrophysiological evidence4 for an involvement of GABA in the action of BZs was presented. The decisive event leading to the discovery of the BZ receptors was a visit to Hoffmann-LaRoche in Basel on July 20, 1976. During this visit, Willy Haefely generously offered to provide me with a sample of [3H]diazepam ([3H]DZP) synthesized at Roche for radiohistochemical studies. On October 21, 1976, I received a gift of 100 mCi [3H]DZP (specific activity 14.5 Ci/mmol) from Hoffman-LaRoche, and a day or two later I did my first experiment with it, which was a complete success.

Keywords

Gaba Receptor Endogenous Ligand Heat Inactivation Hill Number Unheated Control 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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Copyright information

© Springer Science+Business Media New York 1984

Authors and Affiliations

  • Richard F. Squires
    • 1
  1. 1.Nathan S. Kline Institute for Psychiatric ResearchOrangeburgUSA

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